Table 2. Rank summary of the 15 hit compounds evaluated by mouse and human MCs’ degranulation assays.
(Left half) The individual 15 compounds were treated to mouse BMMCs at four different concentrations (100, 50, 25, and 12.5 μM) in Tyrode’s buffer. After 30 min of incubation, collected supernatant was analyzed for percent release of β-hexosaminidase. The ranking order of 15 hit compounds was arranged based on levels of β-hexosaminidase release at 100 μM. (Right half) The individual 15 compounds were treated to human LAD2 cells at four different concentrations (100, 50, 25, and 12.5 μM) in Tyrode’s buffer. After 30 min of incubation, collected supernatant was analyzed for percent release of β-hexosaminidase. The ranking order of 15 hit compounds was arranged based on levels of β-hexosaminidase release at 100 μM.
| Mouse BMMCs | Human LAD2 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rank | Compound Number | % Degranulation at the concentration of compounds | IC50 (μM) | Rank | Compound Number | % Degranulation at the concentration of compounds | IC50 (μM) | ||||||
| 100μM | 50μM | 25μM | 12.5μM | 100μM | 50μM | 25μM | 12.5μM | ||||||
| 1 | ST101036 | 91.1 | 80.3 | 45.1 | 5.8 | 23.5 | 6 | ST101036 | 37.9 | 28.0 | 15.4 | 3.3 | 28.0 |
| 2 | ST081379 | 84.2 | 30.5 | 3.8 | 0 | 65.8 | 3 | ST081379 | 76.0 | 43.0 | 10.2 | 0.8 | 50.1 |
| 3 | R529877 | 80.1 | 13.6 | 0.8 | 0.4 | 70.0 | 4 | R529877 | 49.9 | 5.3 | 0.3 | 0.2 | 75.7 |
| 4 | ST029248 | 72.5 | 41.4 | 32.1 | 25.4 | 515.2 | 2 | ST029248 | 76.8 | 97.2 | 100.0 | 100.0 | 57.9 |
| 5 | ST048871 | 60.0 | 7.9 | 2.8 | 0.4 | 132.7 | 8 | ST048871 | 12.6 | 0.4 | 0.7 | 0.3 | 98.6 |
| 6 | R606278 | 49.6 | 10.0 | 0.3 | 0.5 | 61.9 | 5 | R606278 | 46.8 | 21.4 | 0.2 | 0.1 | 51.2 |
| 7 | R127655 | 29.4 | 14.8 | 7.1 | 3.8 | 129.1 | 10 | R127655 | 7.5 | 4.0 | 2.3 | 1.4 | 295.1 |
| 8 | ST026567 | 27.1 | 13.6 | 2.8 | 0.6 | 54.8 | 1 | ST026567 | 91.3 | 75.7 | 2.9 | 0.4 | 40.5 |
| 9 | ST029279 | 25.8 | 0.3 | 0.3 | 0.3 | 95.1 | 7 | ST029279 | 27.8 | 7.2 | 0.1 | 0.0 | 58.7 |
| 10 | ST099914 | 23.8 | 11.3 | 5.8 | 2.7 | 342.8 | 9 | ST099914 | 9.8 | 4.8 | 2.5 | 1.1 | 352.4 |
| 11 | L201863 | 18.0 | 8.7 | 4.3 | 2.2 | 211.8 | 11 | L201863 | 7.0 | 3.5 | 2.0 | 1.1 | 415.0 |
| 12 | L147192 | 17.7 | 8.3 | 4.2 | 2.0 | 332.7 | 12 | L147192 | 6.2 | 3.2 | 1.6 | 1.1 | 100.9 |
| 13 | ST045940 | 13.6 | 6.9 | 2.7 | 2.2 | 57.7 | 13 | ST045940 | 5.3 | 3.7 | 2.4 | 1.6 | 70.6 |
| 14 | ST086136 | 3.5 | 1.4 | 0.2 | 0.2 | 56.5 | 15 | ST086136 | 1.2 | 0.1 | 0.2 | 0.1 | 104.5 |
| 15 | ST027688 | 1.4 | 0.2 | 0.1 | 0.1 | 264.9 | 14 | ST027688 | 3.0 | 0.5 | 0.6 | 0.4 | 100.0 |